Suntory Limited

Daiichi Suntory Pharma Co., Ltd.

Akira Mizuno

Norio Inomata

Makoto Shibata

Tomoe Iwamori

Tomoe Kamei

Harukazu Fukami

Toshio Tatsuoka

Hidetsura Cho

Takafumi Ishihara

Kyoko Nakanishi

Tetsuo Shimamoto

Mikiko Hamaguchi

Mikiko Miya

Kazuto Sekiuchi

Teruo Muraishi

Takushi Nagata

Keiyu Shima

Masahiro Imoto

Atsuto Ogata

A pyrrolesulfonamide derivative having the following formula (I): wherein the ring P represented by is a pyrrole ring having the following structure: wherein R represents alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Zis not present and Zrepresents H but, when the bond is absent, Zrepresents H and Zrepresents OH or Zand Zare combined together to represent O or a group NOR, in which Rrepresents H, or alkyl, aralkyl or aryl; l stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C&#x2550; or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C&#x2550;; B represents a specific divalent group; Eand Eeach independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.

Pyrrolothiazine and pyrrolothiazepine compounds having serotonin-2 receptor antagonistic and alpha-1-blocking action

Pyrrolothiazine and pyrrolothiazepine compounds having serotonin-2 receptor antagonistic and &agr;-1-blocking action

Pyrroloazepine derivatives

Benzothiazine derivative

Process for production of optically active pyrroloazepine derivatives

A pyrrolesulfonamide compound having formula (I) wherein the ring P represented by &agr; is a pyrrole ring having structure &bgr; or &psgr; wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group &dgr; in which W represents CH, C&boxH; or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C&boxH;; B represents a specific divalent group; E,and E,each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; l stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z,is not present and Z,represents H but, when the bond is absent, Z,represents H and Z,represents OH or Z,and Z,are combined together to represent O or a group NOR,, in which R,represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl. The compound (1) has been improved in potency, selectivity to receptors other than serotonin-2 receptors, toxicity, side effects and/or the like over medicines reported to date and equipped with a &agr;,-blocking action and serotonin-2 receptor antagonistic action in combination.

Disclosed are benzothiazine derivatives represented by the following formula (I):

An intermediate represented by the following formula (XVIII),

Thiopyran derivatives

A method of treating or improving intermittent claudication, which comprises administering, to a patient with intermittent claudication, a pyrroloazepine derivative or a pharmacologically acceptable salt thereof, said pyrroloazepine derivative being represented by the following formula (I):

Intermittent claudication therapeutic drugs comprising pyrroloazepines

A pyrrolesulfonamide derivative having the following formula (I):

A method for treating a circulatory disease or condition in a mammal, which entails administering to the mammal an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof:

Disclosed are pyrroloazepine compounds and their salts. These pyrroloazepine compounds are represented by the following formula:

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Kyoto, Japan

Akira Mizuno